Towards NR2B receptor selective imaging agents for PET-synthesis and evaluation of N-[11C]-(2-methoxy)benzyl (E)-styrene-, 2-naphthyl- and 4-trifluoromethoxyphenylamidine

Erik Årstad; Stefan Platzer; Achim Berthele; Lyn S. Pilowsky; Sajinder K. Luthra; Hans Jürgen Wester; Gjermund Henriksen

doi:10.1016/j.bmc.2006.05.046

Towards NR2B receptor selective imaging agents for PET-synthesis and evaluation of N-[¹¹C]-(2-methoxy)benzyl (E)-styrene-, 2-naphthyl- and 4-trifluoromethoxyphenylamidine

Erik Årstad, Stefan Platzer, Achim Berthele, Lyn S. Pilowsky, Sajinder K. Luthra, Hans Jürgen Wester, Gjermund Henriksen

Research output: Contribution to journal › Article › peer-review

30 Scopus citations

Abstract

Three potent and selective ¹¹C-labelled NR2B antagonists have been synthesized and evaluated as PET ligands. The brain uptake of the compounds in mice varied substantially and was dominated by metabolism. One compound was found to have favourable uptake and retention in the brain, as well as a binding pattern consistent with the expression of the target receptor as measured by in vitro autoradiography. However, the metabolism of the compounds tested was too rapid to allow for in vivo imaging.

Original language	English
Pages (from-to)	6307-6313
Number of pages	7
Journal	Bioorganic and Medicinal Chemistry
Volume	14
Issue number	18
DOIs	https://doi.org/10.1016/j.bmc.2006.05.046
State	Published - 15 Sep 2006

Keywords

Amidine
Carbon-11
Glutamate
NMDA-NR2B
PET

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Årstad, E., Platzer, S., Berthele, A., Pilowsky, L. S., Luthra, S. K., Wester, H. J., & Henriksen, G. (2006). Towards NR2B receptor selective imaging agents for PET-synthesis and evaluation of N-[¹¹C]-(2-methoxy)benzyl (E)-styrene-, 2-naphthyl- and 4-trifluoromethoxyphenylamidine. Bioorganic and Medicinal Chemistry, 14(18), 6307-6313. https://doi.org/10.1016/j.bmc.2006.05.046

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title = "Towards NR2B receptor selective imaging agents for PET-synthesis and evaluation of N-[11C]-(2-methoxy)benzyl (E)-styrene-, 2-naphthyl- and 4-trifluoromethoxyphenylamidine",

abstract = "Three potent and selective 11C-labelled NR2B antagonists have been synthesized and evaluated as PET ligands. The brain uptake of the compounds in mice varied substantially and was dominated by metabolism. One compound was found to have favourable uptake and retention in the brain, as well as a binding pattern consistent with the expression of the target receptor as measured by in vitro autoradiography. However, the metabolism of the compounds tested was too rapid to allow for in vivo imaging.",

keywords = "Amidine, Carbon-11, Glutamate, NMDA-NR2B, PET",

author = "Erik {\AA}rstad and Stefan Platzer and Achim Berthele and Pilowsky, {Lyn S.} and Luthra, {Sajinder K.} and Wester, {Hans J{\"u}rgen} and Gjermund Henriksen",

year = "2006",

month = sep,

day = "15",

doi = "10.1016/j.bmc.2006.05.046",

language = "English",

volume = "14",

pages = "6307--6313",

journal = "Bioorganic and Medicinal Chemistry",

issn = "0968-0896",

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Årstad, E, Platzer, S, Berthele, A, Pilowsky, LS, Luthra, SK, Wester, HJ & Henriksen, G 2006, 'Towards NR2B receptor selective imaging agents for PET-synthesis and evaluation of N-[¹¹C]-(2-methoxy)benzyl (E)-styrene-, 2-naphthyl- and 4-trifluoromethoxyphenylamidine', Bioorganic and Medicinal Chemistry, vol. 14, no. 18, pp. 6307-6313. https://doi.org/10.1016/j.bmc.2006.05.046

Towards NR2B receptor selective imaging agents for PET-synthesis and evaluation of N-[¹¹C]-(2-methoxy)benzyl (E)-styrene-, 2-naphthyl- and 4-trifluoromethoxyphenylamidine. / Årstad, Erik; Platzer, Stefan; Berthele, Achim et al.
In: Bioorganic and Medicinal Chemistry, Vol. 14, No. 18, 15.09.2006, p. 6307-6313.

Research output: Contribution to journal › Article › peer-review

TY - JOUR

T1 - Towards NR2B receptor selective imaging agents for PET-synthesis and evaluation of N-[11C]-(2-methoxy)benzyl (E)-styrene-, 2-naphthyl- and 4-trifluoromethoxyphenylamidine

AU - Årstad, Erik

AU - Platzer, Stefan

AU - Berthele, Achim

AU - Pilowsky, Lyn S.

AU - Luthra, Sajinder K.

AU - Wester, Hans Jürgen

AU - Henriksen, Gjermund

PY - 2006/9/15

Y1 - 2006/9/15

N2 - Three potent and selective 11C-labelled NR2B antagonists have been synthesized and evaluated as PET ligands. The brain uptake of the compounds in mice varied substantially and was dominated by metabolism. One compound was found to have favourable uptake and retention in the brain, as well as a binding pattern consistent with the expression of the target receptor as measured by in vitro autoradiography. However, the metabolism of the compounds tested was too rapid to allow for in vivo imaging.

AB - Three potent and selective 11C-labelled NR2B antagonists have been synthesized and evaluated as PET ligands. The brain uptake of the compounds in mice varied substantially and was dominated by metabolism. One compound was found to have favourable uptake and retention in the brain, as well as a binding pattern consistent with the expression of the target receptor as measured by in vitro autoradiography. However, the metabolism of the compounds tested was too rapid to allow for in vivo imaging.

KW - Amidine

KW - Carbon-11

KW - Glutamate

KW - NMDA-NR2B

KW - PET

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SN - 0968-0896

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EP - 6313

JO - Bioorganic and Medicinal Chemistry

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ER -

Towards NR2B receptor selective imaging agents for PET-synthesis and evaluation of N-[¹¹C]-(2-methoxy)benzyl (E)-styrene-, 2-naphthyl- and 4-trifluoromethoxyphenylamidine

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Keywords

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